L-19 Skeletal Muscle Relaxant

Download as pptx, pdf, or txt
Download as pptx, pdf, or txt
You are on page 1of 26

Skeletal Muscle Relaxants

Dr Naser Ashraf
Types of skeletal muscle relaxants: 2 groups

• Neuromuscular blockers • Spasmolytics

• Relax normal muscles • Reduce spasticity


(surgery and assistance • Centrally acting (except
of ventilation) dantrolene which act on
• No central nervous the skeletal muscle)
system activity. • Used in a variety of
• Used primarily as a part neurologic conditions
of general anesthesia
Skeletal Muscle Relaxants

Neuromuscular
Spasmolytics
blockers
Non-depolarizing
(Competitive)
• D tubocurarine
Centrally Directly
• Pancuronium
acting acting
• Vecuronium
• Atracurium
• Diazepam • Dantrolene
• Mivacurium
• Chlorzoxazone
• Tizanidine
• Baclofen
Depolarizing
(Non-Competitive)
• Succinylcholine
• Decamethomium
Skeletal Muscle contraction
Na+
Na +

Ca

a
2+

a b
ACH
Ac
tio
nP
ote
nti
al

ACH ACH
ACH ACH NMreceptor
ACH

a
ACH

b
ACH
ACH

a
ACH
Motor neuron ACH
ACH
ACH
a
ba ACHEsterase

Skeletal
Muscle
Mechanism of action of
Neuromuscular Blockers
Normal d-Tubocurarine Succinylcholine

Ach A Ch Ach Ach SCh

Ach SCh

Depolarization No Depolarization Persistent Depolarization


Contraction
Repolarization (Fasciculation)

Contraction No contraction Relaxation

Relaxation Flaccid Paralysis


Competitive Antagonists
(Non-depolarizing Blockers)
(Non-depolarizing blockers)

• Long-acting: d tubocurarine,
pancuronium

• Intermediate: Atracurium , vecuronium ,

rocuronium ,
Anti-cholinestrases
(neostigmine, Mechanism of Action
edrophonium) Competitive Antagonism
which preserve
acetylcholine Agonist
are used to reverse
the effect of
d-tubocurarine
Ach Ach
Antagonist
d-Tubocurarine
Affinity : Yes
Intrinsic action : No

NM receptor

Motor End Plate


Actions
• Muscle weakness  Flaccid paralysis
• Order of muscle affected:
– Extrinsic eye muscles, muscles of finger
– Neck muscles (muscles of phonation and swallowing)
– Face
– Hands,
– Feet
– Trunk
– Respiratory muscles (intercostal and diaphragm)
• Recovery in the reverse order
• Consciousness, appreciation of pain not affected
Actions
• Autonomic ganglion blocking property
• Histamine release (by d-tubocurarine)
• CVS
– Significant fall in BP
– Increase in Heart rate
– Vagal gangionic blockade (also ‘ve’ and ‘pan’)
• Newer competitive blockers:
– Negligible effect on BP and HR
Adverse effects
• Hypotension
• Tachycardia
• Respiratory paralysis
• Bronchospasm
• Aspiration of gastric contents
Advantages of synthetic (Newer)
competitive blockers
• Less histamine release
• Do not block autonomic ganglia
• Spontaneous recovery with most of drugs
• Rapacuronium & rocuronium have rapid onset
• Atracuronium: Hoffmans elimination
• Mivacurium short acting
Uses
• As an adjunct to general anaesthesia
– For producing satisfactory skeletal muscle
relaxation
• For facilitating endotracheal intubation
– Rocuronium preferred due to rapid onset of
action
– Succinylcholine is better due to short lasting
duration
Depolarizing Blocker
(Non-competitive Antagonist)
Succinylcholine
One Drug, Two blocks,
Brief and quick,
Genetic variability in metabolism,
Malignant hyperthermia
Skeletal Muscle Relaxants

Quaternary
Succinyl Choline Quaternary
Depolarising muscle relaxants
ammonium ammonium

Two molecules of Acetylcholine)

Acetylcholine
Mechanism of action

Agonist at Nicotinic (NM) receptor


Produces neuromuscular block by overstimulation, end plate is unable to
respond to further stimulation.
Longer lasting or persistent depolarization
Succinylcholine

Actions

• Small rapidly moving muscles (eye, jaw, larynx)


relax before those of limbs and trunks
• Ultimately intercostals and finally diaphragm
paralysis occur  respiratory paralysis
• Recovery in the reverse order
• Muscle relaxation: Onset: within 1 min; peak: 2
min, duration: 5 min; longer duration relaxation
requires continued IV infusion
Succinylcholine
Uses
Suitable for short-term procedures
• Rapid endotracheal intubation during induction of
anaesthesia
• During Electro-Convulsive shock Therapy (ECT)
– To prevent injury
Succinylcholine
Adverse Effects
• Transient Intraocular Tension
• Hyperkalemia : Fasciculations release
potassium in blood
• Succinylcholine apnoea
• Malignant hyperthermia: when used alng
with halothane in general anaesthesia
– Treatment is by rapid cooling of patient &
dantrolene i.v
• Muscle pain
Treatment of succinylcholine
apnoea
• No antidote is available
• Fresh frozen plasma should be infused
• Patient should be ventilated artificially
untill full recovery
Comparison of Competitive and Depolarizing
Blocking Agents
Sr.no Competitive Succinyl choline
1 Competitive blockade Persistant depolarization
2 Non depolarizing Depolarizing
3 Single block Dual block
4 Anticholinesterases Do not reverse
reverse blockade
5 Initial fasciculations not Present
present
6 Slow onset long Rapid onset short
duration duration
7 Release histamine Doesn’t release
Dantrolene
• Directly acting skeletal Muscle relaxant
• Inhibits depolarization induced calcium
release from sarcoplasmic reticulum by
acting on ryanodine receptors
• Drug of choice in malignant hyperthermia
Drug interactions
• Non depolarizing blockers
– Anticholine-esterases (Neostigmine)
• Reverse the action of only non depolarizing
blockers
– Halothane, Aminoglycoside antibiotic like
gentamicin & calcium channel blockers like
nifedipine
• Enhances the neuromuscular blockade
• Depolarizing blockers
– Halothane can cause malignant hyperthermia
Ganglion blockers
• Competitive blockers • Persistant depolarizing
– Hexamethonium – Nicotine large dose
– Trimethaphan
– Mecamylamine
Actions & Adverse effects of ganglion blockers
S.No Organ Dominant ANS Effect/(side effect)of ganglionic
blockade

1. Heart Parasympathetic Tachycardia (Palpitations)


2. Blood vessels Sympathetic Vasodilation (Hypotension)
3. Iris Parasympathetic Mydriasis (Photophobia)
4. Ciliary Muscle Parasympathetic Cycloplegia (Blurring of vision)
5. Intestines Parasympathetic ↓ motility (Constipation)
6. Bladder Parasympathetic ↓ tone (difficulty in micturation)
7. Male sexual function Parasympathetic Inhibition of erection & ejaculation
(Impotence)
8. Salivary Glands Parasympathetic Inhibition of salivation (dry mouth,
difficulty in swallowing)
9. Sweat Glands Sympathetic Inhibition of sweating

You might also like

pFad - Phonifier reborn

Pfad - The Proxy pFad of © 2024 Garber Painting. All rights reserved.

Note: This service is not intended for secure transactions such as banking, social media, email, or purchasing. Use at your own risk. We assume no liability whatsoever for broken pages.


Alternative Proxies:

Alternative Proxy

pFad Proxy

pFad v3 Proxy

pFad v4 Proxy